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Merck
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重要文件

P0115

Sigma-Aldrich

PAC-1

≥98% (HPLC)

同義詞:

1-哌嗪乙酸,2-(苯基甲基)-,[[2-羟基-3-(2-丙烯基)苯基]亚甲基]肼, (4-苄基哌嗪)乙酸(3-烯丙基-2-羟基亚苄基)酰肼

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About This Item

經驗公式(希爾表示法):
C23H28N4O2
CAS號碼:
分子量::
392.49
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

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品質等級

化驗

≥98% (HPLC)

形狀

solid

顏色

white

溶解度

DMSO: ≥10 mg/mL
deionized water: ≤2 mg/mL

儲存溫度

room temp

SMILES 字串

Oc1c(CC=C)cccc1\C=N\NC(=O)CN2CCN(CC2)Cc3ccccc3

InChI

1S/C23H28N4O2/c1-2-7-20-10-6-11-21(23(20)29)16-24-25-22(28)18-27-14-12-26(13-15-27)17-19-8-4-3-5-9-19/h2-6,8-11,16,29H,1,7,12-15,17-18H2,(H,25,28)/b24-16+

InChI 密鑰

YQNRVGJCPCNMKT-LFVJCYFKSA-N

一般說明

蛋白酶激活化合物1(PAC-1)是邻羟基N-酰基肼化合物。[1]它对多种癌细胞具有细胞毒性,例如淋巴瘤,白血病,乳腺癌和胶质母细胞瘤。[2]高剂量的PAC-1可以促进神经兴奋。[2]它有助于作为其他蛋白酶活化化合物原型的蛋白酶原的体外自活化。[3]PAC-1依赖的procaspase-3激活与锌的螯合有关。[1]

生化/生理作用

PAC-1是半胱天冬酶3激活剂。
PAC-1是半胱天冬酶3激活剂。半胱天冬酶激活是癌症治疗中的关键策略。半胱天冬酶3是关键的执行子半胱天冬酶和细胞凋亡的直接效应子。许多癌症的标志是在执行子半胱天冬酶的激活和凋亡反应的丧失中规避信号。半胱天冬酶3激活的EC50=0.33 μM,半胱天冬酶7=4.5 μM。凋亡诱导的IC50=0.92 μM。癌细胞系和组织中半胱天冬酶3水平升高使PAC-1选择性诱导组织中的凋亡。

特點和優勢

该化合物在受体分类和信号转导手册的 半胱天冬酶 页面上有详细描述。如需浏览其他手册页面,请点击此处

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

個人防護裝備

dust mask type N95 (US), Eyeshields, Gloves


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